Volume 7, Issue 2 (2021)                   Pharm Biomed Res 2021, 7(2): 0-0 | Back to browse issues page

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Amini M, Hosseinpoor Tehrani M, Mirshokrayi A, Khobi M. Synthesize of pyrazolo[1,2-b]phthalazine-5,10-dione derivatives: a new class of for α –glucosidase inhibitors. Pharm Biomed Res. 2021; 7 (2)
URL: http://pbr.mazums.ac.ir/article-1-253-en.html
1- Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2- Department of Chemistry, Payame Noor University (PNU), Tehran, Iran
3- Biomaterials Group, The Institue of Pharmaceutical Sciences(TIPS), Tehran University of Medical Sciences, Tehran, Iran
Abstract:   (2619 Views)
Diabetes mellitus is a group of metabolic diseases characterized by hyperglycemia (high blood sugar). α -Glucosidase is a membrane-bound enzyme located at the epithelium of small intestine and catalyzes the final step in the digestion of carbohydrates. Inhibition of α -glucosidase enzyme activity is a reliable approach to control post-prandial hyperglycemia associated risk factors. In this study, a series of Pyrazolo[1,2-b]phthalazine-5,10-dione derivatives 5a–t were synthesized via a multicomponent reaction and evaluated as new inhibitors for α-glucosidase. Four compounds showed higher α-glucosidase inhibitory activity in comparison to standard, acarbose. Among these compounds, compound 5q displayed the most potent α-glucosidase inhibitory activity (IC50 = 155.4 ± 6.0 μM).
 
     
Type of Study: Original Research | Subject: Medical Chemistry

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